Our library of drug research abstracts drawn from the medical literature is updated on a regular schedule, and you can be assured that new ansaid research articles will be listed here shortly after becoming available to us.
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Medical research on ansaid
Development of Enteric Coated Flurbiprofen Tablets using Opadry/acryl-eze System-A Technical Note.
AAPS PharmSciTech. 2008; 9(1): 116-21
Hashmat D, Shoaib MH, Mehmood ZA, Bushra R, Yousuf RI, Lakhani F
Chiral ionic liquids for enantioseparation of pharmaceutical products by capillary electrophoresis.
J Chromatogr A. 2008 Apr 12;
Tran CD, Mejac I
A chiral ionic liquid (IL), S-[3-(chloro-2-hydroxypropyl)trimethylammonium] [bis((trifluoromethyl)sulfonyl)amide] (S-[CHTA](+)[Tf(2)N](-)), which can be easily and readily synthesized in a one-step process from commercially available reagents, can be successfully used both as co-electrolyte and as a chiral selector for CE. A variety of pharmaceutical products including atenolol, propranolol, warfarin, indoprofen, ketoprofen, ibuprofen and flurbiprofen, can be successfully and baseline separated with the use of this IL as electrolyte. Interestingly, while S-[CHTA](+)[Tf(2)N](-) can also serve as a chiral selector, enantioseparation cannot be successfully achieved with S-[CHTA](+)[Tf(2)N](-) as the only chiral selector. In the case of ibuprofen, a second chiral selector, namely a chiral anion (sodium cholate), is needed for the chiral separation. For furbiprofen, in addition to S-[CHTA](+)[Tf(2)N](-) and sodium cholate, a third and neutral chiral selector, 1-S-octyl-beta-d-thioglucopyranoside (OTG), is also needed. Due to the fact that the chirality of this chiral IL resides on the cation (i.e., -[CHTA](+)), and that needed additional chiral selector(s) are either chiral anion (i.e., cholate) or chiral neutral compound (OTG), the results obtained seem to suggest that additional chiral selector(s) are needed to provide the three-point interactions needed for chiral separations.
Determining binding sites of drugs on human serum albumin using FIA-QCM.
Biosens Bioelectron. 2008 Mar 21;
Zhang Q, Huang Y, Zhao R, Liu G, Chen Y
A simple and effective method was developed for determining binding sites of drugs on human serum albumin (HSA) by independent binding or competitive displacement of bilirubin using flow injection analysis-quartz crystal microbalance (FIA-QCM) system. Both independent and competitive bindings were entirely monitored in real time. Bilirubin as a site I-binding ligand was pre-bound to HSA sensor so as to occupy the drug-binding site I. When the model site II-binding drugs (ibuprofen, ketoprofen and flurbiprofen) were injected into the bilirubin pre-bound HSA system, the frequency continuously decreased by 6Hz, 4Hz and 5Hz, respectively, which was the same as that of their individual binding to HSA sensor. It indicated that the drug binding to site II was independent and did not interfere with bilirubin binding. However, when the model site I-binding drugs (iodipamide and magnesium salicylate) were introduced into the system, the frequency remained unchanged in the initial several minutes and then rapidly decreased by 4Hz for iodipamide and increased by 4Hz for magnesium salicylate. This phenomenon revealed site I-binding drugs competitively bound to HSA against bilirubin and displaced the pre-bound bilirubin. The results demonstrate FIA-QCM can be a valid approach for monitoring the dynamic interaction between drugs and HSA in real time further identifying drug-binding sites without the need of labels.
PLGA nanospheres for the ocular delivery of flurbiprofen: Drug release and interactions.
J Pharm Sci. 2008 Apr 18;
Vega E, Gamisans F, García ML, Chauvet A, Lacoulonche F, Egea MA
Poly(D,L-lactide-co-glycolide) nanospheres incorporating flurbiprofen were prepared by the solvent displacement technique for purposes of assessing (i) drug-polymer physicochemical interactions, (ii) flurbiprofen release from the polymer matrix and (iii) eye permeation of the drug formulated in the colloidal system. The resulting nanospheres were on average 200-300 nm in size and bore a negative charge (xi-potential around -25 mV). They were shown by atomic force microscopy and transmission electron microscopy to be spherical and regular in shape. Thermal methods, infrared spectroscopy and X-ray diffraction showed that the drug was dispersed inside the particles. These tests evidenced an eutectic mixture meaning more widespread dispersion of the drug in the polymer system. Entrapped flurbiprofen was released in vitro from the polymer system by dissolution and diffusion in high drug loaded nanospheres, whereas those with a lesser load showed only diffusion. The ex vivo corneal permeation study showed that flurbiprofen-loaded nanospheres enhanced drug penetration by about twofold over commercial eye drops containing poly(vinyl alcohol) and by about fourfold over flurbiprofen in pH 7.4 phosphate buffer. The corneal hydration level of each cornea was determined to evaluate potential corneal damage. (c) 2008 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci.
Optimizing delivery of flurbiprofen to the colon using a targeted prodrug approach.
J Pharm Pharmacol. 2008 May; 60(5): 607-13
Philip AK, Dubey RK, Pathak K
The carboxylic group responsible for the gastric side-effects of the propionic acid derivative, flurbiprofen, was masked temporarily to overcome these side-effects and to accomplish colon-specific delivery of the drug. An amide prodrug (FLU-GLY) was synthesized by coupling flurbiprofen with L-glycine. Confirmation and characterization of the structure of the synthesized prodrug included elemental analysis, Fourier transform (FT)-IR, FT-NMR, mass (FAB) spectroscopy, and determinations of R(f), R(t) and R(M) values, respectively. Aqueous solubility and lipophilicity (logP) value were determined at pH 1.2, 4.0, 6.8 and 7.4. In-vitro reversion of FLU-GLY to flurbiprofen was measured at different pHs and in a simulated colonic environment. Acute toxicity and ulceration potential were evaluated in-vivo in albino rats. Pre-formulation studies showed increased hydrophilicity but a non-significant increase in lipophilicity of the prodrug. In-vitro reversion studies suggested that the prodrug remained intact until colonic pH was attained, when the colonic microfloral enzymes (amidase) hydrolysed the FLU-GLY amide linkage, releasing the free drug. In-vivo evaluation indicated that the prodrug was much less toxic and had less ulcerogenic activity than the parent drug. Selective delivery of drugs to the colon can be useful in terms of reducing the dose administered and reducing undesirable side-effects.
Investigation of nanostructured lipid carriers for transdermal delivery of flurbiprofen.
Drug Dev Ind Pharm. 2008 Apr; 34(4): 453-8
Han F, Li S, Yin R, Shi X, Jia Q
The aim of this study was to develop nanostructured lipid carriers (NLC) for transdermal delivery of Flurbiprofen (FP). The physical stability of FP-NLC and its in vitro permeation profile were investigated. After three months of storage at 4 degrees C, 20 degrees C, and 40 degrees C, no significant differences between the evaluated parameters, such as pH value, the entrapment efficiency, particle size, and zeta potential were observed. In in vitro permeation studies, the cumulative permeated amounts and the release rate from FP-NLC were 412.53 +/- 21.37 mug/cm(2) and 35.25 mug/cm(2)/h after 12 h (n = 6), respectively, while from saturated FP-PBS (pH = 7.4) were 90.83 +/- 8.67 mug/cm(2) and 6.99 mug/cm(2)/h, respectively. These results indicated that the FP-NLC were with good physical stability and were able to improve the permeated amounts and the release rate of FP. It could potentially be exploited as a carrier with improved drug entrapment efficiency and permeated amount in the transdermal delivery of FP.
Eur J Med Chem. 2008 Feb 8;
Kumar H, Javed SA, Khan SA, Amir M
A series of 1,3,4-oxadiazole/thiadiazole and 1,2,4-triazole derivatives of biphenyl-4-yloxy acetic acid were synthesized in order to obtain new compounds with potential anti-inflammatory activity, analgesic activity and lower ulcerogenic potential. All compounds were evaluated for their anti-inflammatory activity by the carrageenan induced rat paw edema test method. The compounds possessing potent anti-inflammatory activity were further tested for their analgesic, ulcerogenic and antioxidant activities. Out of all tested compounds, the compounds 3, 7, 17 and 20, showed significant reduction in rat paw edema induced by carrageenan treatment. These compounds showed significant analgesic effect and at an equimolar oral doses relative to flurbiprofen were also found to be non-gastrotoxic in rats. Compound 17 was evaluated as the lead compound having more anti-inflammatory activity (81.81%) than the reference drug (79.54%), low ulcerogenic potential and protective effect on lipid peroxidation.
Osmotically Regulated Flow of Flurbiprofen through In Situ Formed Asymmetric Membrane Capsule.
Curr Drug Deliv. 2008 Apr; 5(2): 127-32
Philip AK
An in situ formed non-disintegrating controlled release asymmetric membrane capsular system, offering improved osmotic effect, was used to deliver poorly water soluble drug flurbiprofen (model drug) to demonstrate how controlled release characteristics could be manipulated by design of polymeric capsule with an asymmetric membrane. In situ formed asymmetric membrane capsule was made by dry method via precipitation of asymmetric membrane on the walls of hard gelatin capsule. Effect of different formulation variables were studied based on 2(3) factorial design, namely, level of osmogen, ethylcellulose and pore former apart from studying the effect of varying osmotic pressure on drug release. Scanning Electron Microscopy showed an outer dense non porous region and an inner lighter porous region for the prepared asymmetric membrane inside and a gelatin layer outside. Statistical test (Dunnett Multiple Comparison Test) was applied for in vitro drug release at P>0.05. The best formulation closely corresponded to the extra design checkpoint formulation by a similarity (f(2)) value of 96.88. The drug release was independent of pH but dependent on the osmotic pressure of the dissolution medium. The release kinetics followed Higuchi model and mechanism of release was Fickian diffusion.
Impregnation of an intraocular lens for ophthalmic drug delivery.
Curr Drug Deliv. 2008 Apr; 5(2): 102-7
Duarte AR, Simplicio AL, Vega-González A, Subra-Paternault P, Coimbra P, Gil MH, de Sousa HC, Duarte CM
In this work the possibility of impregnating P(MMA-EHA-EGDMA) with flurbiprofen using a clean and environmentally friendly technology, namely supercritical fluid technology was evaluated. P(MMA-EHA-EGDMA) has been proposed as a promising matrix to be used for intraocular delivery of anti-inflammatory drugs used in eye surgery and flurbiprofen is a non-steroidal anti-inflammatory agent. Fundamental studies like, the solubility of the drug in carbon dioxide, as well as the sorption degree of this polymeric matrix in the presence of carbon dioxide have been previously carried out. The aim of this research was to evaluate the effects of these two variables in the impregnation process. Different experimental conditions were tested and the results obtained suggest that the best impregnating conditions for this system are low temperatures and pressures, which at the same time correspond to a lower solubility of the drug in the supercritical fluid and a low swelling of the polymeric matrix. Experiments performed also indicate that the batch impregnation process leads to higher yields of impregnation and according to the release profiles obtained the drug can be released from the matrix up to three months, which presents great advantages for post-surgical treatments.
J Microencapsul. 2008 May; 25(3): 170-8
Coimbra PA, De Sousa HC, Gil MH
Poly(3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) microspheres containing flurbiprofen were prepared by an oil-in-water emulsion solvent evaporation method, in order to develop a particulate drug delivery system for localized administration. A response surface method (RSM) using a central composite design was employed to evaluate the effect of the poly(vinyl alcohol) (PVA) (%, w/v) concentration in the aqueous phase and the PHBV concentration in the organic phase (%, w/v) on some of the resulting microspheres properties. The response variables were the encapsulation efficiency (EE), the mean particle size, the width of particle size distribution (expressed by the SPAN value) and the required time for the in vitro release of 50% of the encapsulated drug (t(50%)). Second-order polynomial and linear equations were fitted to experimental data and were also used to interpret the results. Results indicated that the concentration of the stabilizer (PVA) showed a highly negative effect on the EE probably due to the increased drug solubility in the aqueous phase as a result of the higher PVA concentrations. Particle diameter mean size increased with the increased polymer concentration while the width of the particle size distribution was found to decrease with the increase of the stabilizer agent. Finally, results indicated that none of the investigated variables presented a significant effect on the t(50%) values.